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JPH203 is an inhibitor of L-type amino acid transporter 1 (LAT1; IC50 = 0.14 μM for 14C-leucine uptake in S2 cells expressing the human transporter).1 It is selective for LAT1 over LAT2 (IC50 = >10 μM). JPH203 inhibits 14C-leucine uptake by, and growth of, HT-29 cells (IC50s = 0.06 and 4.1 μM, respectively). It induces apoptosis and increases levels of cleaved caspase-3, caspase-7, caspase-9, and poly(ADP-ribose) polymerase (PARP) in YD-38 oral cancer cells when used at a concentration of 3 mM.2 JPH203 (6.3, 12.5, and 25 mg/kg) reduces tumor growth in an HT-29 mouse xenograft model.1
WARNING This product is not for human or veterinary use.
1. L-
2. JPH203, an L-